JP4837858B2 - 拮抗ホルモン特性を有する、１７β−アシル−１７α−プロピニル−１１β−（環状アミノ）アリールステロイド及びその誘導体 - Google Patents

拮抗ホルモン特性を有する、１７β−アシル−１７α−プロピニル−１１β−（環状アミノ）アリールステロイド及びその誘導体 Download PDF

Info

Publication number
JP4837858B2
JP4837858B2 JP2001522248A JP2001522248A JP4837858B2 JP 4837858 B2 JP4837858 B2 JP 4837858B2 JP 2001522248 A JP2001522248 A JP 2001522248A JP 2001522248 A JP2001522248 A JP 2001522248A JP 4837858 B2 JP4837858 B2 JP 4837858B2
Authority
JP
Japan
Prior art keywords
norpregna
phenyl
diene
propynyl
dione
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2001522248A
Other languages
English (en)
Japanese (ja)
Other versions
JP2003508540A (ja
Inventor
エドガー・シー・クック
ジョン・エー・ケプラー
ジル・エム・オレイリー
Original Assignee
リサーチ・トライアングル・インスティチュート
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by リサーチ・トライアングル・インスティチュート filed Critical リサーチ・トライアングル・インスティチュート
Publication of JP2003508540A publication Critical patent/JP2003508540A/ja
Application granted granted Critical
Publication of JP4837858B2 publication Critical patent/JP4837858B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2001522248A 1999-09-03 2000-09-05 拮抗ホルモン特性を有する、１７β−アシル−１７α−プロピニル−１１β−（環状アミノ）アリールステロイド及びその誘導体 Expired - Fee Related JP4837858B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/389,212 1999-09-03
US09/389,212 US6740645B1 (en) 1999-09-03 1999-09-03 17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties
PCT/US2000/024274 WO2001018025A2 (en) 1999-09-03 2000-09-05 17alpha propynyl 11-aryl steroids

Publications (2)

Publication Number Publication Date
JP2003508540A JP2003508540A (ja) 2003-03-04
JP4837858B2 true JP4837858B2 (ja) 2011-12-14

Family

ID=23537322

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2001522248A Expired - Fee Related JP4837858B2 (ja) 1999-09-03 2000-09-05 拮抗ホルモン特性を有する、１７β−アシル−１７α−プロピニル−１１β−（環状アミノ）アリールステロイド及びその誘導体

Country Status (14)

Country Link
US (1) US6740645B1 (no)
EP (1) EP1208113B1 (no)
JP (1) JP4837858B2 (no)
KR (1) KR100733932B1 (no)
AT (1) ATE431832T1 (no)
AU (1) AU780077B2 (no)
CA (1) CA2384184C (no)
CY (1) CY1109451T1 (no)
DE (1) DE60042238D1 (no)
DK (1) DK1208113T3 (no)
ES (1) ES2326787T3 (no)
NO (1) NO322108B1 (no)
PT (1) PT1208113E (no)
WO (1) WO2001018025A2 (no)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0900234T3 (da) 1996-05-01 2000-11-06 Us Gov Health & Human Serv 21-substituerede progesteronderivater anvendt som nye antigestagener
US6900193B1 (en) 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
CA2403756C (en) * 2000-03-17 2010-02-09 Hyun K. Kim Structural modification of 19-norprogesterone i: 17-.alpha.-substituted, 11-.beta.-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
AU2004217988C1 (en) * 2003-02-28 2010-06-03 Southwest Foundation For Biomedical Research Method for preparing 17 alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates thereof, and methods for the preparation of such intermediates
TWI477276B (zh) 2008-04-28 2015-03-21 Repros Therapeutics Inc 抗黃體素給藥方案
KR102166867B1 (ko) * 2010-03-22 2020-10-19 앨러간 파마슈티컬스 인터내셔널 리미티드 항프로게스틴의 비독성 전달을 위한 조성물들과 그 방법들
CN103130862B (zh) * 2011-11-30 2016-04-13 成都伊诺达博医药科技有限公司 醋酸乌利司他关键中间体3,20-双(亚乙二氧基)-19-去甲孕甾-5,9-二烯-17-醇的合成方法
ES2701400T3 (es) 2012-05-31 2019-02-22 Repros Therapeutics Inc Formulaciones para la administración vaginal de antiprogestinas
EP2914268B1 (en) 2012-11-02 2018-07-04 Repros Therapeutics Inc. Methods and compositions for treating progesterone-dependent conditions
WO2016090139A1 (en) * 2014-12-03 2016-06-09 Evestra, Inc. Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer
CN115521352B (zh) * 2022-11-01 2024-05-14 湖南新合新生物医药有限公司 一种甲基双烯醇酮的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4954490A (en) * 1988-06-23 1990-09-04 Research Triangle Institute 11 β-substituted progesterone analogs
WO1997041145A1 (en) * 1996-05-01 1997-11-06 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL122740A (en) 1997-01-15 2003-09-17 Akzo Nobel Nv 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them
US5952319A (en) 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4954490A (en) * 1988-06-23 1990-09-04 Research Triangle Institute 11 β-substituted progesterone analogs
US5073548A (en) * 1988-06-23 1991-12-17 Research Triangle Institute 11 β-substituted progesterone analogs
WO1997041145A1 (en) * 1996-05-01 1997-11-06 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents

Also Published As

Publication number Publication date
NO20021037L (no) 2002-04-05
DE60042238D1 (de) 2009-07-02
AU780077B2 (en) 2005-02-24
PT1208113E (pt) 2009-08-25
CY1109451T1 (el) 2014-08-13
WO2001018025A3 (en) 2001-09-20
CA2384184A1 (en) 2001-03-15
ATE431832T1 (de) 2009-06-15
AU7111300A (en) 2001-04-10
ES2326787T3 (es) 2009-10-20
KR100733932B1 (ko) 2007-07-03
NO322108B1 (no) 2006-08-14
JP2003508540A (ja) 2003-03-04
CA2384184C (en) 2008-07-08
US6740645B1 (en) 2004-05-25
EP1208113A2 (en) 2002-05-29
DK1208113T3 (da) 2009-08-31
WO2001018025A2 (en) 2001-03-15
EP1208113B1 (en) 2009-05-20
NO20021037D0 (no) 2002-03-01
EP1208113A4 (en) 2003-01-02
KR20020092906A (ko) 2002-12-12

Similar Documents

Publication Publication Date Title
JP4563578B2 (ja) アゴニスト又はアンタゴニストホルモン特性を有する２０−ケト−１１β−アリールステロイドとその誘導体
JP2000503980A (ja) 新規１９―ノル−プレグネン誘導体類
JP4545930B2 (ja) アゴニストまたはアンタゴニストホルモン特性を有する１７β−ニトロ−１１β−アリルステロイドとその誘導体
JP4837858B2 (ja) 拮抗ホルモン特性を有する、１７β−アシル−１７α−プロピニル−１１β−（環状アミノ）アリールステロイド及びその誘導体
RU2230071C2 (ru) Гормональные или негормональные стероидные соединения, способ терапевтического лечения
JP4545929B2 (ja) アゴニストまたはアンタゴニストホルモン特性を有する１７β−アミノおよびヒドロキシルアミノ−１１β−アリルステロイドとその誘導体
JP4768181B2 (ja) １１β−アリール−１７，１７−スピロチオラン置換ステロイド
CA2614667C (en) 20-keto-11.beta.-arylsteroids and their derivatives having agonist or antagonist hormonal properties

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070822

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101026

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110126

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20110315

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110715

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20110726

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110830

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110929

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20141007

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees